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Merck

658552

Tyrphostin AG 1478

≥98% (HPLC), epidermal growth factor receptor kinase inhibitor, solid

Synonyme(s) :

AG 1478, 4-(3-Chloroanilino)-6,7-dimethoxyquinazoline

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About This Item

Formule empirique (notation de Hill) :
C16H14ClN3O2
Numéro CAS:
175178-82-2
Poids moléculaire :
315.75
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
MFCD00270914

Nom du produit

AG 1478, A cell-permeable, reversible, ATP-competitive, highly potent and selective inhibitor of epidermal growth factor receptor kinase versus HER2-neu and platelet-derived growth factor receptor kinase.

SMILES string

Clc1cc(ccc1)Nc2ncnc3c2cc(c(c3)OC)OC

InChI

1S/C16H14ClN3O2/c1-21-14-7-12-13(8-15(14)22-2)18-9-19-16(12)20-11-5-3-4-10(17)6-11/h3-9H,1-2H3,(H,18,19,20)

InChI key

GFNNBHLJANVSQV-UHFFFAOYSA-N

assay

≥98% (HPLC)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
protect from light

color

pale yellow

solubility

DMSO: 5 mg/mL

shipped in

ambient

storage temp.

−20°C

Quality Level

100

Catégories apparentées

Biochem/physiol Actions

Cell permeable: yes
Primary Target
Epidermal growth factor receptor kinase
Product competes with ATP.
Reversible: yes
Target IC50: 3 nM against epidermal growth factor receptor kinase

Disclaimer

Toxicity: Standard Handling (A)

General description

A cell-permeable, reversible, ATP-competitive, highly potent and selective inhibitor of epidermal growth factor receptor kinase (IC50 = 3 nM) versus HER2-neu (IC50 >100 µM) and platelet-derived growth factor receptor kinase (IC50 >100 µM). Abolishes MAP kinase (ERK) activation induced by Angiotensin II (Cat. No. 05-23-0101). Also inhibits the activation of EGFR kinase and MAP kinase by 4-hydroxynonenal. Downregulates ARF1 activity and disperses Golgi structure. A 10 mM (1 mg/317 µl) solution of AG 1478 (Cat. No. 658548) in DMSO is also available.

Legal Information

Sold under license of U.S. Patent 5,457,105 and European Patent 0,566,266.
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

Pan, H., et al. 2008. J. Biol. Chem.283, In press.
Liu, W., et al. 1999. J. Cell Sci.112, 2409.
Eguchi, S., et al. 1998. J. Biol. Chem. 273, 8890.
Levitzki, A., and Gazit, A. 1995. Science267, 1782.
Fry, D.W., et al. 1994. Science265, 1093.
Osherov, N., and Levitski, A. 1994. Eur. J. Biochem.225, 1047.
Ward, W.H., et al. 1994. Biochem. Pharmacol.48, 659.

Preparation Note

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Further dilute with aqueous buffers just prior to use.

Classe de stockage

11 - Combustible Solids

wgk

WGK 3

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Alessandro Brombin et al.
Cell reports, 38(2), 110234-110234 (2022-01-13)
Melanocytes, the pigment-producing cells, are replenished from multiple stem cell niches in adult tissue. Although pigmentation traits are known risk factors for melanoma, we know little about melanocyte stem cell (McSC) populations other than hair follicle McSCs and lack key
S P Soltoff
The Journal of biological chemistry, 273(36), 23110-23117 (1998-08-29)
The activation of growth factor receptors and receptors coupled to heterotrimeric guanine nucleotide-binding proteins (G-proteins) can increase mitogen-activated protein (MAP) kinase activity in many cells. Previously, we demonstrated that the activation of G-protein-coupled P2Y2 receptors by extracellular ATP and UTP
Tong San Tan et al.
Journal of cell science, 134(19) (2021-10-14)
In the skin fragility disorder epidermolysis bullosa simplex (EBS), mutations in keratin 14 (K14, also known as KRT14) or keratin 5 (K5, also known as KRT5) lead to keratinocyte rupture and skin blistering. Severe forms of EBS are associated with
Zachary M Harris et al.
Oxidative medicine and cellular longevity, 2022, 9518592-9518592 (2022-10-05)
Studies have linked severe hyperoxia, or prolonged exposure to very high oxygen levels, with worse clinical outcomes. This study investigated the role of epidermal growth factor receptor (EGFR) in hyperoxia-induced lung injury at very high oxygen levels (>95%). Effects of
Akito Kakiuchi et al.
Oncology reports, 45(4) (2021-03-03)
In human head and neck squamous cell carcinoma (HNSCC), the invasion and metastatic properties of cancer cells are promoted by junctional adhesion molecule‑A (JAM‑A) and claudin‑1; these are epithelial tight junction molecules regulated by histone deacetylases (HDACs) and transcription factor
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